Projects funded by the NCN

Information on the principal investigator and host institution

Information of the project and the call

Keywords

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Analysis and evaluation of the effectiveness of anorexic and safety properties for the new histamine H3 receptor ligands

2016/23/B/NZ7/01063

Keywords:

H3 histamine receptor ligands anorexic properties obesity

Descriptors:

  • NZ7_14: Pharmacy, pharmacotherapy, pharmacology
  • NZ4_6: Endocrinology
  • NZ7_12: Prevention of human diseases

Panel:

NZ7 - Diagnostic tools, therapies and public health: public health, epidemiology, environmental health risks and occupational medicine, medical ethics, drug discovery and therapies, pharmacology

Host institution :

Uniwersytet Jagielloński Collegium Medicum, Collegium Medicum, Wydział Farmaceutyczny

woj. małopolskie

Other projects carried out by the institution 

Principal investigator (from the host institution):

dr hab. Magdalena Kotańska 

Number of co-investigators in the project: 7

Call: OPUS 12 - announced on 2016-09-15

Amount awarded: 632 100 PLN

Project start date (Y-m-d): 2017-07-14

Project end date (Y-m-d): 2021-07-13

Project duration:: 48 months (the same as in the proposal)

Project status: Project settled

Project description

Download the project description in a pdf file

Note - project descriptions were prepared by the authors of the applications themselves and placed in the system in an unchanged form.

Equipment purchased [PL]

  1. Zamrażarka - 80 st.C (45 000 PLN)
  2. Komputer z drukarką i z oprogramowaniem (569 PLN)
  3. Mieszadło magnetyczne z grzaniem i termometrem dotykowym.
  4. Dozownik reagentów do multifunkcjonalnego czytnika płytek reakcyjnych (UV-VIS Fluostar Optima Spectrofotometr) (2 szt.) (30 000 PLN)
  5. Mieszadło magnetyczne z grzaniem i termometrem dotykowym (4 500 PLN)
  6. Zestaw bloków grzewczych do mieszadeł magnetycznych (13 000 PLN)

Information in the final report

  • Publication in academic press/journals (8)
  1. Structural modifications and in vitro pharmacological evaluation of 4-pyridyl-piperazine derivatives as an active and selective histamine H3 receptor ligands.
    Authors:
    Szczepańska K, Karcz T, Siwek A, Kuder KJ, Latacz G, Bednarski M, Szafarz M, Hagenow S, Lubelska A, Olejarz-Maciej A, Sobolewski M, Mika K, Kotańska M, Stark H, Kieć-Kononowicz K.
    Academic press:
    Bioorganic Chemistry (rok: 2019, tom: 91, strony: 103071), Wydawca: Elservier
    Status:
    Published
    DOI:
    10.1016/j.bioorg.2019.103071. - link to the publication
  2. Synthesis and biological activity of novel tert-butyl and tert-pentylphenoxyalkyl piperazine derivatives as histamine H3R ligands
    Authors:
    Szczepańska K, Karcz T, Mogilski S, Siwek A, Kuder KJ, Latacz G, Kubacka M, Hagenow S, Lubelska A, Olejarz A, Kotańska M, Sadek B, Stark H, Kieć-Kononowicz K.
    Academic press:
    European Journal of Medicinal Chemistry (rok: 2018, tom: 152, strony: 223-234), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.ejmech.2018.04.043 - link to the publication
  3. KSK19 - Novel histamine H3 receptor ligand reduces body weight in diet induced obese mice.
    Authors:
    Kotańska M, Mika K, Reguła K, Szczepańska K, Szafarz M, Bednarski M, Olejarz-Maciej A, Nowak K, Latacz G, Mogilski S, Kuder KJ, Kieć-Kononowicz K, Sapa J.
    Academic press:
    Biochemical Pharmacology (rok: 2019, tom: 168, strony: 193-203), Wydawca: Elservier
    Status:
    Published
    DOI:
    10.1016/j.bcp.2019.07.006. - link to the publication
  4. Optimization and preclinical evaluation of novel histamine H3 receptor ligands: Acetyl and propionyl phenoxyalkyl piperazine derivatives
    Authors:
    Szczepańska K, Karcz T, Kotańska M, Siwek A, Kuder KJ, Latacz G, Mogilski S, Hagenow S, Lubelska A, Sobolewski M, Stark H, Kieć-Kononowicz K
    Academic press:
    Biooranic & Medicinal Chemistry (rok: 2018, tom: 26, strony: 6056-6066), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.bmc.2018.11.010 - link to the publication
  5. Structural modifications in the distal, regulatory region of histamine H 3 receptor antagonists leading to the identification of a potent anti-obesity agent
    Authors:
    Katarzyna Szczepańska, Steffen Pockes, Sabina Podlewska, Carina Höring, Kamil Mika, Gniewomir Latacz, Marek Bednarski, Agata Siwek, Tadeusz Karcz, Martin Nagl, Merlin Bresinsky, Denise Mönnich, Ulla Seibel, Kamil J Kuder, Magdalena Kotańska, Holger Stark, Sigurd Elz, Katarzyna Kieć-Kononowicz
    Academic press:
    Eur J Med Chem (rok: 2021, tom: 213, strony: 113041), Wydawca: Elservier
    Status:
    Published
    DOI:
    10.1016/j.ejmech.2020.113041 - link to the publication
  6. Metabolic benefits of novel histamine H 3 receptor ligands in the model of excessive eating: The importance of intrinsic activity and pharmacokinetic properties
    Authors:
    Mika K, Szafarz M, Bednarski M, Kuder K, Szczepańska K, Pociecha K, Pomierny B, Kieć-Kononowicz K, Sapa J, Kotańska M.
    Academic press:
    Biomedicine and Pharmacotherapy (rok: 2021, tom: 142, strony: 111952), Wydawca: Elservier
    Status:
    Published
    DOI:
    10.1016/j.biopha.2021.111952 - link to the publication
  7. Discovery of Potential, Dual-Active Histamine H 3 Receptor Ligands with Combined Antioxidant Properties
    Authors:
    Kuder KJ, Kotańska M, Szczepańska K, Mika K, Reiner-Link D, Stark H, Kieć-Kononowicz K.
    Academic press:
    Molecules (rok: 2021, tom: 26, strony: 2300), Wydawca: MDPI
    Status:
    Published
    DOI:
    10.3390/molecules26082300 - link to the publication
  8. Influence of betahistine repeated administration on a weight gain and selected metabolic parameters in the model of excessive eating in rats
    Authors:
    Mika K, Szafarz M, Sapa J, Kotańska M.
    Academic press:
    Biomedicine and Pharmacotherapy (rok: 2021, tom: 141, strony: 111892), Wydawca: Elservier
    Status:
    Published
    DOI:
    10.1016/j.biopha.2021.111892 - link to the publication

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